US5240923AExpiredUtility

Sulfonamides useful as carbonic anhydrase inhibitors

91
Assignee: ALCON LAB INCPriority: Apr 9, 1990Filed: Oct 9, 1991Granted: Aug 31, 1993
Est. expiryApr 9, 2010(expired)· nominal 20-yr term from priority
A61P 9/12A61P 43/00C07D 333/34C07D 513/04C07D 333/38A61P 27/02C07D 409/04C07D 495/04C07D 409/12
91
PatentIndex Score
78
Cited by
13
References
14
Claims

Abstract

Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.

Claims

exact text as granted — not AI-modified
We claim: 
     
       1. A compound selected from the group consisting of: 3,4-Dihydro-2-(2-methoxy)ethyl-4-propylamino-2H- thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide;   2-(2-Ethoxyethyl-)-4-ethylamino-3,4-dihydro-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide;   2-(2-Ethoxy)ethyl-3,4-dihydro-4-propylamino-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide;   4-Ethylamino-3,4-dihydro-2-(3-methoxy)propyl-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide;   3,4-Dihydro-2-(3-methoxy)propyl-4-propylamino-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide;   3,4-Dihydro-2-[2-(methoxyethoxy)ethyl]-4-propylamino-2H-thieno[3,2-e]-1,2-thiazine-6-syulfonamide 1,1-dioxide; Ethylamino-3,4-dihydro-2-[2-(methoxyethoxy)ethyl]-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide;   4-Ethylamino-3,4-dihydro-2-[3-(methoxyethoxy)propyl]-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide; and   3,4-Dihydro-2-[3-(methoxyethoxy)propyl]-4-propylamino-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide.   
     
     
       2. The compound of claim 10 which is 3,4-Dihydro-2-(2-methoxy)ethyl-4-propylamino-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide.   
     
     
       3. The Compound of claim 1 which is 4-Ethylamino-3,4-dihydro-2-(3-methoxy)propyl-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide -1,1-dioxide. 
     
     
       4. R-(+)-4-Ethylamino-3,4-dihydro-2-(2-methoxy)ethyl-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide. 
     
     
       5. R-(+)-3,4-Dihydro-2-(2-methoxy)ethyl-4-propylamino-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide. 
     
     
       6. A formulation for controlling intraocular pressure comprising a therapeutically effective amount of the compound of claim 1 in a pharmaceutically acceptable carrier. 
     
     
       7. The formulation of claim 6 wherein the compound concentration is between about 0.1 and 10% by weight. 
     
     
       8. A formulation for controlling intraocular pressure comprising a therapeutically effective amount of the compound of claim 4 in a pharmaceutically acceptable carrier. 
     
     
       9. The formulation of claim 8 wherein the compound concentration is between about 0.1 and 10% by weight. 
     
     
       10. The formulation of claim 9 wherein the concentration is between about 0.25 wt % and 5.0 wt %. 
     
     
       11. A formulation for controlling intraocular pressure comprising a therapeutically effective amount of the Compound of claim 5 in a pharmaceutically acceptable carrier. 
     
     
       12. The formulation of claim 11 wherein the compound concentration is between about 0.1 and 10% by weight. 
     
     
       13. The formulation of claim 12 wherein the concentration is between about 0.25 wt % and 5.0 wt %. 
     
     
       14. A method for controlling intraocular pressure which comprises topically administering to the affected eye a therapeutically effective amount of the compound of claim 1.

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